EP2421867A4 - Piperidine inhibitors of janus kinase 3 - Google Patents

Piperidine inhibitors of janus kinase 3

Info

Publication number
EP2421867A4
EP2421867A4 EP20100767652 EP10767652A EP2421867A4 EP 2421867 A4 EP2421867 A4 EP 2421867A4 EP 20100767652 EP20100767652 EP 20100767652 EP 10767652 A EP10767652 A EP 10767652A EP 2421867 A4 EP2421867 A4 EP 2421867A4
Authority
EP
European Patent Office
Prior art keywords
janus kinase
piperidine
inhibitors
piperidine inhibitors
janus
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
EP20100767652
Other languages
German (de)
French (fr)
Other versions
EP2421867B1 (en
EP2421867A2 (en
Inventor
Tadimeti S Rao
Chengzhi Zhang
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Auspex Pharmaceuticals Inc
Original Assignee
Auspex Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Auspex Pharmaceuticals Inc filed Critical Auspex Pharmaceuticals Inc
Priority to EP15002523.7A priority Critical patent/EP3026052A1/en
Publication of EP2421867A2 publication Critical patent/EP2421867A2/en
Publication of EP2421867A4 publication Critical patent/EP2421867A4/en
Application granted granted Critical
Publication of EP2421867B1 publication Critical patent/EP2421867B1/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/04—Artificial tears; Irrigation solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
EP10767652.0A 2009-04-20 2010-04-20 Piperidine inhibitors of janus kinase 3 Active EP2421867B1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP15002523.7A EP3026052A1 (en) 2009-04-20 2010-04-20 Preparation of deuterated piperidine inhibitors of janus kinase 3

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US17085809P 2009-04-20 2009-04-20
US30088710P 2010-02-03 2010-02-03
PCT/US2010/031773 WO2010123919A2 (en) 2009-04-20 2010-04-20 Piperidine inhibitors of janus kinase 3

Related Child Applications (1)

Application Number Title Priority Date Filing Date
EP15002523.7A Division EP3026052A1 (en) 2009-04-20 2010-04-20 Preparation of deuterated piperidine inhibitors of janus kinase 3

Publications (3)

Publication Number Publication Date
EP2421867A2 EP2421867A2 (en) 2012-02-29
EP2421867A4 true EP2421867A4 (en) 2012-10-10
EP2421867B1 EP2421867B1 (en) 2015-09-02

Family

ID=43011721

Family Applications (2)

Application Number Title Priority Date Filing Date
EP10767652.0A Active EP2421867B1 (en) 2009-04-20 2010-04-20 Piperidine inhibitors of janus kinase 3
EP15002523.7A Withdrawn EP3026052A1 (en) 2009-04-20 2010-04-20 Preparation of deuterated piperidine inhibitors of janus kinase 3

Family Applications After (1)

Application Number Title Priority Date Filing Date
EP15002523.7A Withdrawn EP3026052A1 (en) 2009-04-20 2010-04-20 Preparation of deuterated piperidine inhibitors of janus kinase 3

Country Status (10)

Country Link
US (4) US8299084B2 (en)
EP (2) EP2421867B1 (en)
JP (3) JP5709276B2 (en)
KR (1) KR20130009577A (en)
CN (2) CN104817561B (en)
AU (2) AU2010239396B2 (en)
BR (1) BRPI1007737A2 (en)
CA (2) CA3025627C (en)
ES (1) ES2552805T3 (en)
WO (1) WO2010123919A2 (en)

Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2421867B1 (en) 2009-04-20 2015-09-02 Auspex Pharmaceuticals, Llc Piperidine inhibitors of janus kinase 3
US20120195966A1 (en) * 2011-01-27 2012-08-02 Frank Sievert Oral dosage form for modified release comprising a jak3 inhibitor
EP2481411A1 (en) * 2011-01-27 2012-08-01 Ratiopharm GmbH Oral dosage forms for modified release comprising the JAK3 inhibitor tasocitinib
ES2659763T3 (en) 2011-02-14 2018-03-19 The Regents Of The University Of Michigan Compositions and procedures for the treatment of obesity and related disorders
US20150291594A1 (en) * 2012-08-14 2015-10-15 Concert Pharmaceuticals, Inc. Deuterated Ponatinib
CN102875555A (en) * 2012-09-27 2013-01-16 同济大学 Synthetic method of JAK (janus kinase) inhibitor Tofacitinib
EP2935216B1 (en) * 2012-12-17 2018-06-27 Sun Pharmaceutical Industries Limited Process for the preparation of tofacitinib and intermediates thereof
US9757529B2 (en) 2012-12-20 2017-09-12 Otitopic Inc. Dry powder inhaler and methods of use
US9757395B2 (en) 2012-12-20 2017-09-12 Otitopic Inc. Dry powder inhaler and methods of use
US9670160B2 (en) 2012-12-28 2017-06-06 Glenmark Pharmaceuticals Limited Process for the preparation of tofacitinib and intermediates thereof
EP2943489B1 (en) 2013-01-09 2018-04-11 Concert Pharmaceuticals Inc. Deuterated momelotinib
ME03780B (en) 2013-01-15 2021-04-20 Incyte Holdings Corp Thiazolecarboxamides and pyridinecarboxamide compounds useful as pim kinase inhibitors
CN103965114B (en) * 2013-01-28 2016-01-06 苏州泽璟生物制药有限公司 Deuterated phenyl amino pyrimidine compounds and comprise the pharmaceutical composition of this compound
CN103073552B (en) * 2013-02-05 2015-08-12 华润赛科药业有限责任公司 A kind of unformed Citric Acid holder method is for the preparation method of Buddhist nun
JP6041823B2 (en) 2013-03-16 2016-12-14 ファイザー・インク Tofacitinib oral sustained release dosage form
EP3607941A1 (en) 2013-04-30 2020-02-12 Otitopic Inc. Dry powder formulations and methods of use
EP2991647B1 (en) 2013-05-02 2019-04-24 The Regents Of The University Of Michigan Deuterated amlexanox with improved metabolic stability
US20160122354A1 (en) * 2013-06-05 2016-05-05 Srinivasan Thirumalai Rajan PROCESS FOR THE PREPARATION OF (3R,4R)-4-METHYL-3-(METHYL-7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL-AMINO)-ß-OXO-1-PIPERIDINEPROPANENITRILE AND ITS SALTS
CN104447752A (en) * 2013-09-16 2015-03-25 天津市汉康医药生物技术有限公司 Tofacitinib hydrate and preparation method thereof
CN104447751A (en) * 2013-09-16 2015-03-25 天津市汉康医药生物技术有限公司 Tofacitinib compound
CN104292231B (en) * 2013-09-17 2016-11-30 广东东阳光药业有限公司 A kind of citric acid expelling pathogens by strengthening vital QI is for the preparation method of Buddhist nun
CN104513248B (en) * 2013-09-30 2019-05-24 重庆医药工业研究院有限责任公司 A kind of purification process of tropsch imatinib intermediate
CN105873931B (en) * 2013-10-08 2018-10-16 广东东阳光药业有限公司 Support method replaces cloth citrate
CN103819474A (en) * 2013-11-04 2014-05-28 湖南华腾制药有限公司 Preparation method of tofacitinib
HUE053975T2 (en) * 2013-12-09 2021-08-30 Unichem Lab Ltd An improved process for the preparation of (3r,4r)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine
EP3102190A4 (en) 2014-02-07 2017-09-06 Auspex Pharmaceuticals, Inc. Novel pharmaceutical formulations
US20150284327A1 (en) * 2014-04-04 2015-10-08 Auspex Pharmaceuticals, Inc. Oxindole inhibitors of tyrosine kinase
CN104710346B (en) * 2015-02-15 2017-04-12 江苏苏利精细化工股份有限公司 Method for synthesizing cis-1-benzyl-3-methylamino-4-methyl-piperidine
EP3078665A1 (en) * 2015-04-10 2016-10-12 OLON S.p.A. Efficient method for the preparation of tofacitinib citrate
EA036063B1 (en) * 2015-05-29 2020-09-22 Уси Форчун Фармасьютикал Ко., Лтд Janus kinase inhibitor
TWI734699B (en) 2015-09-09 2021-08-01 美商英塞特公司 Salts of a pim kinase inhibitor
TW201718546A (en) 2015-10-02 2017-06-01 英塞特公司 Heterocyclic compounds useful as PIM kinase inhibitors
CN105440039A (en) * 2015-11-24 2016-03-30 山东淄博新达制药有限公司 Synthesis method of tofacitinib citrate
US10214536B2 (en) 2016-01-29 2019-02-26 The Regents Of The University Of Michigan Amlexanox analogs
CN105884781B (en) * 2016-04-18 2018-04-20 山东罗欣药业集团股份有限公司 Preparation method of tofacitinib citrate
CN106188064A (en) * 2016-07-07 2016-12-07 国药集团容生制药有限公司 A kind of preparation method of N methyl N ((3R, 4R) 4 picoline 3 base) 7H pyrrolo-[2,3 d] pyrimidine 4 amine
CN105949204A (en) * 2016-07-25 2016-09-21 国药集团容生制药有限公司 Preparation method of N-((3R, 4R)-1-benzyl-4-methyl pyridine-3-yl)-N-methyl-7H-pyrrolo-[2, 3-d] pyrimidine-4-amine
EP3421455B1 (en) * 2017-06-29 2019-03-27 F.I.S.- Fabbrica Italiana Sintetici S.p.A. Improved process for the preparation of chiral 3-amino-piperidins, useful intermediates for the preparation of tofacitinib
CN109293682A (en) * 2017-07-25 2019-02-01 重庆医药工业研究院有限责任公司 A kind of support method is for cloth impurity and preparation method thereof
EP3684338A4 (en) 2017-09-22 2021-06-23 Otitopic Inc. Dry powder compositions with magnesium stearate
US10786456B2 (en) 2017-09-22 2020-09-29 Otitopic Inc. Inhaled aspirin and magnesium to treat inflammation
CN108358930A (en) * 2018-02-05 2018-08-03 南京法恩化学有限公司 A kind of preparation method of citric acid tropsch imatinib
CN109776547A (en) * 2019-03-22 2019-05-21 北京新领先医药科技发展有限公司 Preparation method of tofacitinib citrate
CN111848496B (en) * 2020-07-28 2021-10-08 湖南华纳大药厂手性药物有限公司 Preparation method of tofacitinib intermediate amine and double hydrochloride thereof
CN112679508B (en) * 2021-03-09 2021-08-10 正大天晴药业集团南京顺欣制药有限公司 Preparation method of tofacitinib intermediate
WO2023248010A2 (en) 2022-06-23 2023-12-28 Synovo Gmbh Targeted modulators of jak3 for treatment of inflammatory and autoimmune diseases

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001042246A2 (en) * 1999-12-10 2001-06-14 Pfizer Products Inc. PYRROLO[2,3-d]PYRIMIDINE COMPOUNDS

Family Cites Families (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20040068613A (en) 1994-03-25 2004-07-31 이소테크니카 인코포레이티드 Deuterated compound and composition for treating hypertension
US6221335B1 (en) 1994-03-25 2001-04-24 Isotechnika, Inc. Method of using deuterated calcium channel blockers
AU3607895A (en) * 1994-09-30 1996-04-26 Novartis Ag 1-acyl-4-aliphatylaminopiperidine compounds
JP4666762B2 (en) 1998-06-19 2011-04-06 ファイザー・プロダクツ・インク Pyrrolo [2.3-d] pyrimidine compounds
PA8474101A1 (en) 1998-06-19 2000-09-29 Pfizer Prod Inc PYROLEUM [2,3-D] PIRIMIDINE COMPOUNDS
US6440710B1 (en) 1998-12-10 2002-08-27 The Scripps Research Institute Antibody-catalyzed deuteration, tritiation, dedeuteration or detritiation of carbonyl compounds
ES2193921T3 (en) 1999-12-03 2003-11-16 Pfizer Prod Inc SULFAMOILHETEROARIL-PIRAZOL COMPOUNDS AS ANTINFLAMATORY / ANALGESIC AGENTS.
EP1134290A3 (en) 2000-03-14 2004-01-02 Pfizer Products Inc. Pharmacophore models for the identification of the CYP2D6 inhibitory potency of selective serotonin reuptake inhibitors
PT1294724E (en) 2000-06-26 2006-07-31 Pfizer Prod Inc COMPOUNDS PYRROLE (2,3-D) PYRIMIDINE AS IMMUNOSPRESSOR AGENTS
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
GT200200234A (en) 2001-12-06 2003-06-27 NEW CRYSTAL COMPOUNDS
TW200413273A (en) 2002-11-15 2004-08-01 Wako Pure Chem Ind Ltd Heavy hydrogenation method of heterocyclic rings
EP1572649A2 (en) * 2002-11-21 2005-09-14 Pfizer Products Inc. 3-amino-piperidine derivatives and processes for their preparation
JP2006509000A (en) 2002-11-26 2006-03-16 ファイザー・プロダクツ・インク Method of treatment of graft rejection
WO2005051393A1 (en) 2003-11-25 2005-06-09 Pfizer Products Inc. Method of treatment of atherosclerosis
EP1734967A2 (en) 2003-12-17 2006-12-27 Pfizer Products Incorporated Pyrrolo [2,3-d] pyrimidine compounds for treating transplant rejection
WO2005063318A1 (en) 2003-12-17 2005-07-14 Pfizer Products Inc. Stent with therapeutically active drug coated thereon
US20050137679A1 (en) 2003-12-17 2005-06-23 Pfizer Inc Modified stent useful for delivery of drugs along stent strut
WO2005063251A1 (en) 2003-12-17 2005-07-14 Pfizer Products Inc. Modified stent useful for delivery of drugs along stent strut
JP2007536310A (en) 2004-05-03 2007-12-13 ノバルティス アクチエンゲゼルシャフト Combination comprising S1P receptor agonist and JAK3 kinase inhibitor
WO2006013114A1 (en) 2004-08-06 2006-02-09 Develogen Aktiengesellschaft Use of a timp-2 secreted protein product for preventing and treating pancreatic diseases and/or obesity and/or metabolic syndrome
US20090156602A1 (en) 2004-11-24 2009-06-18 Nigel Graham Cooke Organic Compounds
US7968535B2 (en) 2005-05-04 2011-06-28 Develogen Atkiengesellschaft Use of azapaullones for preventing and treating pancreatic autoimmune disorders
EP1885454A2 (en) 2005-05-04 2008-02-13 DeveloGen Aktiengesellschaft Use of gsk-3 inhibitors for preventing and treating pancreatic autoimmune disorders
WO2006136374A2 (en) 2005-06-20 2006-12-28 Develogen Aktiengesellschaft Use of gip and/or vitamin d3 analogues thereof for enhancing stem or progenitor cell differentiation into insulin producing cells
AU2006273762A1 (en) 2005-07-29 2007-02-01 Pfizer Products Inc. Pyrrolo[2,3-d]pyrimidine derivatives; their intermediates and synthesis
US20080033011A1 (en) 2005-07-29 2008-02-07 Concert Pharmaceuticals Inc. Novel benzo[d][1,3]-dioxol derivatives
US7750168B2 (en) 2006-02-10 2010-07-06 Sigma-Aldrich Co. Stabilized deuteroborane-tetrahydrofuran complex
GB0605691D0 (en) 2006-03-21 2006-05-03 Novartis Ag Organic Compounds
WO2008029237A2 (en) * 2006-09-05 2008-03-13 Pfizer Products Inc. Combination therapies for rheumatoid arthritis
AR066016A1 (en) 2007-04-11 2009-07-15 Alcon Res Ltd USE OF AN ALFA TNF INHIBITOR TOGETHER WITH AN ANTIHISTAMINE TO TREAT ALLERGIC RHINITIS AND ALLERGIC CONJUNCTIVITIS
US20090182035A1 (en) 2007-04-11 2009-07-16 Alcon Research, Ltd. Use of a combination of olopatadine and cilomilast to treat non-infectious rhinitis and allergic conjunctivitis
CN101743009A (en) 2007-07-11 2010-06-16 辉瑞大药厂 Pharmaceutical compositions and methods of treating dry eye disorders
MX2010012457A (en) 2008-05-13 2010-12-07 Irm Llc Fused nitrogen containing heterocycles and compositions thereof as kinase inhibitors.
RS54560B1 (en) 2008-06-10 2016-06-30 Abbvie Inc. Tricyclic compounds
EP2421867B1 (en) 2009-04-20 2015-09-02 Auspex Pharmaceuticals, Llc Piperidine inhibitors of janus kinase 3

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001042246A2 (en) * 1999-12-10 2001-06-14 Pfizer Products Inc. PYRROLO[2,3-d]PYRIMIDINE COMPOUNDS

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
C. PRAKASH ET AL: "Metabolism, Pharmacokinetics and Excretion of a Janus Kinase-3 Inhibitor, CP-690,550, in Healthy Male Volunteers", (AMERICAN ASSOCIATION OF PHARMACEUTICAL SCIENTISTS) AAPS JOURNAL, 1 January 2008 (2008-01-01), XP055036773, Retrieved from the Internet <URL:http://www.aapsj.org/abstracts/AM_2008/AAPS2008-002492.PDF> [retrieved on 20120830] *
FOSTER A B: "Deuterium isotope effects in the metabolism of drugs and xenobiotics: implications for drug design", ADVANCES IN DRUG RESEARCH, ACADEMIC PRESS, LONDON, GB, vol. 14, 1 January 1985 (1985-01-01), pages 1 - 40, XP009086953, ISSN: 0065-2490 *
See also references of WO2010123919A2 *

Also Published As

Publication number Publication date
AU2016206214A1 (en) 2016-08-11
JP5932080B2 (en) 2016-06-08
WO2010123919A3 (en) 2011-03-03
US8962638B2 (en) 2015-02-24
JP5709276B2 (en) 2015-04-30
ES2552805T3 (en) 2015-12-02
US8299084B2 (en) 2012-10-30
EP2421867B1 (en) 2015-09-02
CN104817561A (en) 2015-08-05
CA2759026C (en) 2019-01-15
JP6145534B2 (en) 2017-06-14
KR20130009577A (en) 2013-01-23
US9856261B2 (en) 2018-01-02
EP3026052A1 (en) 2016-06-01
US20100291026A1 (en) 2010-11-18
CA3025627C (en) 2021-08-31
CA2759026A1 (en) 2010-10-28
AU2010239396A1 (en) 2011-11-03
CA3025627A1 (en) 2010-10-28
CN102459270B (en) 2015-04-29
US20160340361A1 (en) 2016-11-24
US20150322070A1 (en) 2015-11-12
EP3026052A9 (en) 2016-12-07
AU2016206214B2 (en) 2017-11-23
US9493469B2 (en) 2016-11-15
AU2010239396B2 (en) 2016-06-23
WO2010123919A2 (en) 2010-10-28
CN102459270A (en) 2012-05-16
JP2012524085A (en) 2012-10-11
EP2421867A2 (en) 2012-02-29
US20130040974A1 (en) 2013-02-14
JP2015129164A (en) 2015-07-16
BRPI1007737A2 (en) 2015-09-01
CN104817561B (en) 2017-06-13
JP2016175919A (en) 2016-10-06

Similar Documents

Publication Publication Date Title
EP2421867A4 (en) Piperidine inhibitors of janus kinase 3
IL216511A0 (en) Janus kinase inhibitor compounds and methods
IL218271A0 (en) Heterocyclic compounds as janus kinase inhibitors
HRP20130787T1 (en) Imidazopyridazinecarbonitriles useful as kinase inhibitors
HRP20130698T1 (en) Novel phenylpyrazinones as kinase inhibitors
EP2278969A4 (en) Inhibitors of janus kinases
ZA201004942B (en) Ptrrolopyrazine kinase inhibitors
EP2299816A4 (en) Inhibitors of janus kinases
ZA201004055B (en) 4-pyrazolyl-n-arylpyrimidin-2-amines and 4-pyrazolyl-n-heteroarylpyrimidin-2-amines as janus kinase inhibitors
EP2346508A4 (en) Heterocyclic kinase inhibitors
EP2166846A4 (en) Inhibitors of janus kinases
EP2231143A4 (en) Inhibitors of janus kinases
ZA201003429B (en) Inhibitors of c-fms kinase
HK1151291A1 (en) 2-benzylpyridazinone derivatives as met kinase inhibitors
EP2310384A4 (en) Inhibitors of janus kinases
IL210573A0 (en) Compounds as kinase inhibitors
IL220205A0 (en) Heterocyclic compounds as janus kinase inhibitors
EP2341775A4 (en) Inhibitors of janus kinases
EP2200612A4 (en) Inhibitors of janus kinases
EP2231152A4 (en) Thienopyranones as kinase inhibitors
HK1156611A1 (en) Naphthyridininones as aurora kinase inhibitors aurora

Legal Events

Date Code Title Description
PUAI Public reference made under article 153(3) epc to a published international application that has entered the european phase

Free format text: ORIGINAL CODE: 0009012

17P Request for examination filed

Effective date: 20111110

AK Designated contracting states

Kind code of ref document: A2

Designated state(s): AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO SE SI SK SM TR

DAX Request for extension of the european patent (deleted)
A4 Supplementary search report drawn up and despatched

Effective date: 20120906

RIC1 Information provided on ipc code assigned before grant

Ipc: A61P 19/02 20060101ALI20120831BHEP

Ipc: C07D 487/04 20060101AFI20120831BHEP

Ipc: A61P 37/02 20060101ALI20120831BHEP

Ipc: C07D 403/12 20060101ALI20120831BHEP

17Q First examination report despatched

Effective date: 20130527

GRAP Despatch of communication of intention to grant a patent

Free format text: ORIGINAL CODE: EPIDOSNIGR1

INTG Intention to grant announced

Effective date: 20150326

GRAS Grant fee paid

Free format text: ORIGINAL CODE: EPIDOSNIGR3

GRAA (expected) grant

Free format text: ORIGINAL CODE: 0009210

AK Designated contracting states

Kind code of ref document: B1

Designated state(s): AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO SE SI SK SM TR

REG Reference to a national code

Ref country code: GB

Ref legal event code: FG4D

REG Reference to a national code

Ref country code: AT

Ref legal event code: REF

Ref document number: 746526

Country of ref document: AT

Kind code of ref document: T

Effective date: 20150915

Ref country code: CH

Ref legal event code: EP

REG Reference to a national code

Ref country code: IE

Ref legal event code: FG4D

REG Reference to a national code

Ref country code: DE

Ref legal event code: R096

Ref document number: 602010027213

Country of ref document: DE

REG Reference to a national code

Ref country code: ES

Ref legal event code: FG2A

Ref document number: 2552805

Country of ref document: ES

Kind code of ref document: T3

Effective date: 20151202

Ref country code: NL

Ref legal event code: FP

REG Reference to a national code

Ref country code: AT

Ref legal event code: MK05

Ref document number: 746526

Country of ref document: AT

Kind code of ref document: T

Effective date: 20150902

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: FI

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20150902

Ref country code: GR

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20151203

Ref country code: LT

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20150902

Ref country code: LV

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20150902

Ref country code: NO

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20151202

REG Reference to a national code

Ref country code: LT

Ref legal event code: MG4D

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: PL

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20150902

Ref country code: SE

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20150902

Ref country code: AT

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20150902

Ref country code: HR

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20150902

REG Reference to a national code

Ref country code: FR

Ref legal event code: PLFP

Year of fee payment: 7

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: CZ

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20150902

Ref country code: IS

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20160102

Ref country code: SK

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20150902

Ref country code: EE

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20150902

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: RO

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20150902

Ref country code: PT

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20160104

REG Reference to a national code

Ref country code: DE

Ref legal event code: R097

Ref document number: 602010027213

Country of ref document: DE

PLBE No opposition filed within time limit

Free format text: ORIGINAL CODE: 0009261

STAA Information on the status of an ep patent application or granted ep patent

Free format text: STATUS: NO OPPOSITION FILED WITHIN TIME LIMIT

26N No opposition filed

Effective date: 20160603

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: SI

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20150902

Ref country code: DK

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20150902

Ref country code: BE

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20160430

REG Reference to a national code

Ref country code: CH

Ref legal event code: PL

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: BE

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20150902

Ref country code: LU

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20160420

REG Reference to a national code

Ref country code: IE

Ref legal event code: MM4A

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: CH

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20160430

Ref country code: LI

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20160430

REG Reference to a national code

Ref country code: FR

Ref legal event code: PLFP

Year of fee payment: 8

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: IE

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20160420

REG Reference to a national code

Ref country code: FR

Ref legal event code: PLFP

Year of fee payment: 9

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: SM

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20150902

Ref country code: HU

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT; INVALID AB INITIO

Effective date: 20100420

Ref country code: CY

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20150902

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: MT

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20160430

Ref country code: MK

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20150902

Ref country code: TR

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20150902

Ref country code: MC

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20150902

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: BG

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20150902

P01 Opt-out of the competence of the unified patent court (upc) registered

Effective date: 20230525

PGFP Annual fee paid to national office [announced via postgrant information from national office to epo]

Ref country code: NL

Payment date: 20240320

Year of fee payment: 15

PGFP Annual fee paid to national office [announced via postgrant information from national office to epo]

Ref country code: GB

Payment date: 20240321

Year of fee payment: 15

PGFP Annual fee paid to national office [announced via postgrant information from national office to epo]

Ref country code: IT

Payment date: 20240320

Year of fee payment: 15

Ref country code: FR

Payment date: 20240320

Year of fee payment: 15

PGFP Annual fee paid to national office [announced via postgrant information from national office to epo]

Ref country code: DE

Payment date: 20240320

Year of fee payment: 15

PGFP Annual fee paid to national office [announced via postgrant information from national office to epo]

Ref country code: ES

Payment date: 20240502

Year of fee payment: 15